期刊
NATURE STRUCTURAL & MOLECULAR BIOLOGY
卷 22, 期 6, 页码 506-U101出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/nsmb.3029
关键词
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资金
- US National Institutes of Health Mental Health (NIH-MH) R. Kirschstein postdoctoral fellowship
- Brain and Behavior Research Foundation Young Investigator research award
- postdoctoral fellowship from the American Heart Association
- NIH-MH
- Methamphetamine Abuse Research Center of the Oregon Health & Science University [P50DA018165]
- Howard Hughes Medical Institute
Most antidepressants elicit their therapeutic benefits through selective blockade of Na+/Cl--coupled neurotransmitter transporters. Here we report X-ray structures of the Drosophila melanogaster dopamine transporter in complexes with the polycyclic antidepressants nisoxetine or reboxetine. The inhibitors stabilize the transporter in an outward-open conformation by occupying the substrate-binding site. These structures explain how interactions between the binding pocket and substituents on the aromatic rings of antidepressants modulate drug-transporter selectivity.
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